Crebinostat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Crebinostat 是一种新型认知增强剂，可抑制 I 类 HDAC/1/2/3。

Crebinostat is a novel cognitive enhancer that inhibits class I HDAC/1/2/3 (IC50=0.7/1.0/2.0 nM), class IIb HDAC6 (IC50=9.3 nM) with weaker inhibition of the class I HDAC8 and no significant inhibition of the class IIa HDAC/4/5/7/9; potently induces acetylation of both histone H3 and histone H4 as well as enhanced the expression of the CREB target gene Egr1 in cultured mouse primary neurons; upregulates Bdnf and Grn, and downregulates Mapt (tau) gene expression-genes; brain penetrant.(In Vitro):Crebinostat (1 μM; 24 h) induces acetylation of AcH4K12 and AcH3K9 in mouse primary neuronal cells.Crebinostat (1 μM; 24 h) downregulates Mapt mRNA expression, and upregulates Hspa1b (Hsp70) and Bdnf mRNA expression in mouse primary cultured neurons.Crebinostat (1 μM; 24 h) increases histone acetylation and synapsin I punctae along dendrites in primary cultured neurons.(In Vivo):Crebinostat (25 mg/kg; IP; for 10 days) enhances memory of contextual fear conditioning in mice; induces an increase in total hippocampal acetylation of H4K12 and H3K9.

Crebinostat (1 μM; 24 h) induces acetylation of AcH4K12 and AcH3K9 in mouse primary neuronal cells.Crebinostat (1 μM; 24 h) downregulates Mapt mRNA expression, and upregulates Hspa1b (Hsp70) and Bdnf mRNA expression in mouse primary cultured neurons.Crebinostat (1 μM; 24 h) increases histone acetylation and synapsin I punctae along dendrites in primary cultured neurons. Western Blot Analysis Cell Line:Mouse primary neuronal cells (dissociated from E17 embryonic mouse forebrain) Concentration:1 μM Incubation Time:24 h Result:Induced robust acetylation of AcH4K12 and AcH3K9 in a dose dependent manner with EC50s of 0.29 μM and 0.18 μM.

Crebinostat (25 mg/kg; IP; for 10 days) enhances memory of contextual fear conditioning in mice; induces an increase in total hippocampal acetylation of H4K12 and H3K9. Animal Model:Male C57BL/6J mice (9-10 weeks)Dosage:25 mg/kg Administration:IP; alternate daily between left and right sides of the abdomen, for 10 days Result:Enhanced memory of contextual fear conditioning in mice; induced a trend towards an increase in total hippocampal acetylation of both H4K12 and H3K9.

Crebinostat

Cell Cycle/DNA Damage

HDAC

HDAC

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1092061-61-4

353.422

C20H23N3O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (282.96 mM)

O=C(NO)CCCCCC(N/N=C/C1=CC=C(C2=CC=CC=C2)C=C1)=O

Heptanoic acid,7-(hydroxyamino)-7-oxo-,2-([1,1'-biphenyl]-4-ylmethylene)hydrazide

(-20℃)

With Ice Pack

≥ 2 years